L 28 Opioids Flashcards by Mac Mac | Brainscape

Q

What are the Endogenous Opioids?

A

Endorphins
Enkephalins

Dynorphins
Endomorphins

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Endomorphins receptor?

A

Mu

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Dynorphins receptor?

A

Kappa

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Enkephalins receptor?

A

Delta

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Heroine is converted to?

A

Morphine

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Difference between Heroin and Morphine?

A

Heroin= 2-4x more potent

crosses BBB faster

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

What drug is available as a suppository?

A

Hydromorphone

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Hydromorphone potency? duration?

A

Hydro=
8-10x more potent
shorter duration

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

What drug is the same as hydromorphone?

A

Oxymorphone

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Codeine potency? efficacy?

A

Codeine=
1/10 the potency of morphine
lower efficacy

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

What is Codeine converted to?

A

morphine

-> by CYP450 2D6

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Oxycodone potency?

A

10x potency of Codeine

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

What mixtures contain Codeine?

A

Acetaminophen

NSAID

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

What are the Synthetic Compounds?

A

Meperidine

Fentanyl

Methadone

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Meperidine potency? Duration?

A

1/8th potency of morphine

short

How well did you know this?

1

Not at all

2

3

4

5

Perfectly

Q

Meperidine SE?

A

toxic metabolite builds up

= seizures

Q

Advantages of Meperidine?

A

dec SM spasms than Morphine

no miosis

Q

Fentanyl potency? Onset? Duration?

A

80-100x potency of morphine

fast onset

short duration

Q

How is Fentanyl administered?

A

I.v. for anesthesia

Q

Methadone potency?

A

I.v. potency similar to morphine

oral= 4x more potency

Q

Methadone Tx?

A

narcotic dependence

Q

Methadone duration?

A

inc w/ repeated use

Q

What are the Opioid Antagonists?

A

Naloxone
Naltrexone

Methylnaltrexone
Naloxagol

Q

What are signs of OD?

A

stupor, coma

RR low

pinpoint pupils

low body temp

placid SM, jaw relaxed

Q

Naloxone efficacy?

A

not effective orally

Q

Naltrexone efficacy?

A

effective orally or injected

Q

Methylnaltrexone Tx?

A

opioid induced constipation

Q

Methylnaltrexone quaternary?

A

doesn’t cross BBB

Q

Naloxegol Tx?

A

opioid induced constipation

Q

What are the Mixed Agonist-Antagonist drugs?

A

Butorphanol

Nalbuphine

Q

Butorphanol MOA? Available as?

A

Kappa agonist
Mu antagonist

nasal spray

Q

Butorphanol potency?

A

5x more potent in women

Q

Nalbuphine MOA?

A

Kappa agonist

Mu antagonist

Q

Nalbuphine advantages?

A

little dysphoria compared to nalorphine

less abuse potential than morphine

Q

Tramadol MOA?

A

Mu & Delta agonist

(-) reuptake of NE, SE

a2 adreno agonist

Q

Tapentadol MOA?

A

Mu & Delta agonist

(-) NE reuptake

Q

What drugs have actions that are synergistic for analgesia? and are antidepressant?

A

Tramadol

Tapentadol